Dexmedetomidine hydrochloride(Synonyms: 盐酸右美托咪定; (+)-Medetomidine hydrochloride; (S)-Medetomidine hydrochloride)

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Dexmedetomidine hydrochloride (Synonyms: 盐酸右美托咪定; (+)-Medetomidine hydrochloride; (S)-Medetomidine hydrochloride) 纯度: 99.39%

Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) 是一种有效，选择性和具有口服活性的 α2 肾上腺素能受体 (α2-adrenoceptor) 激动剂，Ki 值为 1.08 nM。Dexmedetomidine hydrochloride 对 α1 肾上腺素受体显示出 1620 倍的选择性。Dexmedetomidine hydrochloride 具有抗焦虑作用，可用于促进安定和缓解疼痛的研究。

Dexmedetomidine hydrochloride(Synonyms: 盐酸右美托咪定; (+)-Medetomidine hydrochloride; (S)-Medetomidine hydrochloride)

Dexmedetomidine hydrochloride Chemical Structure

CAS No. : 145108-58-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥500 In-stock
5 mg ￥400 In-stock
10 mg ￥550 In-stock
50 mg ￥1800 In-stock
100 mg   询价  
200 mg   询价  

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生物活性

Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects[1][2][3].

IC50 & Target

α2-adrenergic receptor

1.08 nM (IC50)

体外研究
(In Vitro)

Medetomidine has high selectivity for α2 adrenoceptors (Ki=1.08 nM) over α1 adrenoceptors (Ki=1750 nM) in rat brain membranes as measured by the displacement of [3H]clonidine[1].
Medetomidine (0.1-100 nM) inhibits the twitch response in field-stimulated mouse vas deferens, with a pD2 of 9.0[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Medetomidine (10-100 μg/kg; i.v. at 5-min intervals) produces a dose-dependent pupillary dilatation in pentobarbitone-anaesthetized rats[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Sprague-Dawley rats (270-350 g)[1]
Dosage: 1, 5, 10, 50, 100 mg/kg
Administration: I.v. at 5-min intervals
Result: Produced the pupil dilatation of 2.5 mm (approximately half of the maximum effect) at the cumulative dose of 4 μg/kg.

Clinical Trial

分子量

236.74

Formula

C13H17ClN2
CAS 号

145108-58-3
中文名称

盐酸右美托咪定
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (1056.01 mM; Need ultrasonic)

H2O : ≥ 50 mg/mL (211.20 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.2240 mL 21.1202 mL 42.2404 mL
5 mM 0.8448 mL 4.2240 mL 8.4481 mL
10 mM 0.4224 mL 2.1120 mL 4.2240 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (8.79 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.79 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (8.79 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.79 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (8.79 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.79 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Virtanen R, et, al. Characterization of the selectivity, specificity and potency of medetomidine as an alpha 2-adrenoceptor agonist. Eur J Pharmacol. 1988 May 20;150(1-2):9-14.

    [2]. Gertler R, et, al. Dexmedetomidine: a novel sedative-analgesic agent. Proc (Bayl Univ Med Cent). 2001 Jan;14(1):13-21.

    [3]. Sajid B, et, al. A comparison of oral dexmedetomidine and oral midazolam as premedicants in children. J Anaesthesiol Clin Pharmacol. Jan-Mar 2019;35(1):36-40.

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